Abstract
Plasma glucose is continuously filtered through the glomerulus and then is reabsorbed via the transcellular transport system of proximal tubules in the kidney. The glucose reabsorption system in the kidney is mediated by sodiumdependent glucose cotransporters (SGLTs). Most of filtered glucose is reabsorbed by the low affinity, high capacity SGLT2 located in the proximal renal tubule. SGLT2 inhibitors, such as T-1095, enhance urinary glucose excretion and consequently lower blood glucose levels independent of insulin action. The principle behind SGLT inhibition involves the amelioration of diabetic conditions without increasing body weight and the risk of hypoglycemia. A number of SGLT2 inhibitors are being developed for the treatment of diabetes. This review offers the summary of structure-activity relationships (SARs) and pharmacological profiles of T-1095 and diverse SGLT2 inhibitors.
Keywords: SGLT, anti-diabetic agent, urinary glucose excretion, diabetes mellitus, phlorizin, T-1095, remogliflozin etabonate, sergliflozin, dapagliflozin
Current Topics in Medicinal Chemistry
Title: Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitors for New Anti-Diabetic Agent
Volume: 10 Issue: 4
Author(s): Sumihiro Nomura
Affiliation:
Keywords: SGLT, anti-diabetic agent, urinary glucose excretion, diabetes mellitus, phlorizin, T-1095, remogliflozin etabonate, sergliflozin, dapagliflozin
Abstract: Plasma glucose is continuously filtered through the glomerulus and then is reabsorbed via the transcellular transport system of proximal tubules in the kidney. The glucose reabsorption system in the kidney is mediated by sodiumdependent glucose cotransporters (SGLTs). Most of filtered glucose is reabsorbed by the low affinity, high capacity SGLT2 located in the proximal renal tubule. SGLT2 inhibitors, such as T-1095, enhance urinary glucose excretion and consequently lower blood glucose levels independent of insulin action. The principle behind SGLT inhibition involves the amelioration of diabetic conditions without increasing body weight and the risk of hypoglycemia. A number of SGLT2 inhibitors are being developed for the treatment of diabetes. This review offers the summary of structure-activity relationships (SARs) and pharmacological profiles of T-1095 and diverse SGLT2 inhibitors.
Export Options
About this article
Cite this article as:
Nomura Sumihiro, Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitors for New Anti-Diabetic Agent, Current Topics in Medicinal Chemistry 2010; 10 (4) . https://dx.doi.org/10.2174/156802610790980567
DOI https://dx.doi.org/10.2174/156802610790980567 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Recent Advances in the Development of Casein Kinase 1 Inhibitors
Current Medicinal Chemistry Trends in Mitochondrial Therapeutics for Neurological Disease
Current Medicinal Chemistry Pituitary Dysfunction as a Cause of Cardiovascular Disease
Current Pharmaceutical Design Curcuminoids in Neurodegenerative Diseases
Recent Patents on CNS Drug Discovery (Discontinued) Anti-Vascular Endothelial Growth Factor Drug Treatment of Diabetic Macular Edema: The Evolution Continues
Current Diabetes Reviews Human Cognitive and Neuro-Psychiatric Bio-Markers in the Cardiac Peri-Operative Patient
Current Molecular Medicine Solvent-Free Synthesis of 4,5-Dihydropyrano[c]chromene Derivatives Over TiO<sub>2</sub> Nanoparticles as an Economical and Efficient Catalyst
Current Catalysis Albumin Competitively Inhibits Glycation of Less Abundant Proteins
Protein & Peptide Letters Reversal of Bone Cancer Pain by HSV-1-Mediated Silencing of CNTF in an Afferent Area of the Spinal Cord Associated with AKT-ERK Signal Inhibition
Current Gene Therapy Bioinformatics and Protein Design
Current Pharmaceutical Biotechnology The Small Heat Shock Protein HspB8: Role in Nervous System Physiology and Pathology
CNS & Neurological Disorders - Drug Targets Gene Therapy in Peripheral Nerve Reconstruction Approaches
Current Gene Therapy Inflammatory Mechanisms and Redox Status in Periodontal and Cardiometabolic Diseases: Effects of Adjunctive Nutritional Antioxidants and Statins
Infectious Disorders - Drug Targets Antioxidative Activity, Polyphenolic Content and Anti-Glycation Effect of Some Thai Medicinal Plants Traditionally Used in Diabetic Patients
Medicinal Chemistry The Interaction of Depression and Diabetes: A Review
Current Diabetes Reviews Pulmonary Complications in Diabetes Mellitus: The Role of Glycemic Control
Current Drug Targets - Inflammation & Allergy The Endocrine Regulation of Stem Cells: Physiological Importance and Pharmacological Potentials for Cell-Based Therapy
Current Stem Cell Research & Therapy Challenge of Mesenchymal Stem Cells Against Diabetic Foot Ulcer
Current Stem Cell Research & Therapy Oxidative stress in carcinogenesis: new synthetic compounds with dual effects upon free radicals and cancer.
Current Medicinal Chemistry Neuroprotective Effects of Tetracyclines: Molecular Targets, Animal Models and Human Disease
CNS & Neurological Disorders - Drug Targets